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Unopened flower buds of Capparis spinosa L. (capers), generally used in the Mediterranean area as food flavoring, are known to be a good source of bioactive compounds. The aim of this work was to evaluate the nutraceutical value of salt‐fermented capers collected from different areas of Pantelleria Island (Italy), testing their methylglyoxal and glyoxal trapping capacity and antioxidant activity by 2,2‐diphenyl‐1‐picryl hydrazyl (DPPH), [2,2‐azinobis(3‐ethylben‐ zothiazoline‐6‐sulfonic acid)] diammonium salt (ABTS), and oxygen radical absorbance capacity (ORAC) assays. Hydrophilic extracts were also characterized by high‐performance liquid chromatography–electrospray ionization/mass spectrometry. Among 24 detected compounds, several flavonol derivatives and glucosinolates were identified. The levels of kaempferol and quercetin derivatives varied considerably among the five accessions considered (6.46 to 267.93 and 22.39 to 367.14 mg kaempferol and quercetin equivalent /g fresh weight, respectively), with kaempferol derivatives more representative than quercetin ones. Person's coefficient indicated a high correlation between total phenolic content and anti‐DPPH radical capacity (R2 = 0.665), as well as between total flavonoid content and antioxidant capacity (by ORAC assay; R2 = 0.888) and between total flavonoid content and glyoxal and methylglyoxal trapping capacity (R2 = 0.918). Results indicate that capers from Pantelleria Island represent a rich source of bioactive compounds with potential nutraceutical relevance. Practical Application The findings of this study highlight the health benefits of Pantelleria capers consumption due to their composition in antioxidants and their biological properties (antiradical and alpha‐dicarbonyls trapping) correlated with the development of a high number of chronic–degenerative diseases. These results are also important for the agricultural and commercial sectors involved in the production of capers from Pantelleria, which received the Protected Geographical Indications recognition.

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